N-Substituted pyrazole-3-carboxamides as inhibitors of human 15-lipoxygenase. Issue 15 (1st August 2015)

• Record Type: Journal Article
• Authors: Pelcman, Benjamin; Sanin, Andrei; Nilsson, Peter; Schaal, Wesley; Olofsson, Kristofer; Krog-Jensen, Christian; Forsell, Pontus; Hallberg, Anders; Larhed, Mats; Boesen, Thomas; Kromann, Hasse; Claesson, Hans-Erik
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 15(2015)
• Page Start: 3017
• Page End: 3023
• Publication Date: 2015-08-01
• Subjects: 15-Lipoxygenase -- Inhibitors -- Arachidonic acid -- Pyrazole; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.05.007
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: High-throughput screening was used to find selective inhibitors of human 15-lipoxygenase-1 (15-LOX-1). One hit, a 1-benzoyl substituted pyrazole-3-carboxanilide (1a ), was used as a starting point in a program to develop potent and selective 15-LOX-1 inhibitors.